Pertuzumab (Perjeta)

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General information

Class/mechanism: Humanized monoclonal antibody that binds to the extracellular dimerization subdomain II of HER2, preventing dimerization with other HER receptors (i.e. EGFR/HER1, HER3, and HER4). Pertuzumab inhibits ligand-initiated intracellular signaling via the MAP (mitogen-activated protein) kinase and PI3K (phosphoinositide 3-kinase) pathways, which results in cell growth arrest and apoptosis. Also stimulates antibody-dependent cell-mediated cytotoxicity (ADCC).[1][2][3]
Route: IV
Extravasation: no information

For conciseness and simplicity, currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the package insert.[1]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

  • 6/8/2012: FDA approved for use in combination with trastuzumab and docetaxel for the treatment of patients with HER2-positive metastatic breast cancer who have not received prior anti-HER2 therapy or chemotherapy for metastatic disease. (Based on CLEOPATRA)
  • 9/30/2013: Granted accelerated approval for use in combination with trastuzumab and docetaxel for the neoadjuvant treatment of patients with HER2-positive, locally advanced, inflammatory, or early stage breast cancer (either greater than 2 cm in diameter or node positive) as part of a complete treatment regimen for early breast cancer. (Approval extended to the neoadjuvant setting; based on NeoSphere, TRYPHAENA, BERENICE)
  • 12/20/2017: Regular FDA approval for use in combination with trastuzumab and chemotherapy as adjuvant treatment of patients with HER2-positive early breast cancer at high risk of recurrence. (Granted regular approval; Approval extended to the adjuvant setting; based on APHINITY)

History of changes in EMA indication

  • 3/4/2013: Initial marketing authorization as Perjeta.

Also known as

  • Code names: 2C4, Rhumab 2C4.
  • Brand names: Omnitarg, Perjeta